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Identification of 2,4-Disubstituted Imidazopyridines as Hemozoin Formation Inhibitors with Fast-Killing Kinetics and In Vivo Efficacy in the Plasmodium falciparum NSG Mouse Model.
Horatscheck, André; Andrijevic, Ana; Nchinda, Aloysius T; Le Manach, Claire; Paquet, Tanya; Khonde, Lutete Peguy; Dam, Jean; Pawar, Kailash; Taylor, Dale; Lawrence, Nina; Brunschwig, Christel; Gibhard, Liezl; Njoroge, Mathew; Reader, Janette; van der Watt, Mariëtte; Wicht, Kathryn; de Sousa, Ana Carolina C; Okombo, John; Maepa, Keletso; Egan, Timothy J; Birkholtz, Lyn-Marie; Basarab, Gregory S; Wittlin, Sergio; Fish, Paul V; Street, Leslie J; Duffy, James; Chibale, Kelly.
Affiliation
  • Horatscheck A; Drug Discovery and Development Centre (H3D), Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
  • Andrijevic A; Drug Discovery and Development Centre (H3D), Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
  • Nchinda AT; Drug Discovery and Development Centre (H3D), Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
  • Le Manach C; Drug Discovery and Development Centre (H3D), Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
  • Paquet T; Drug Discovery and Development Centre (H3D), Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
  • Khonde LP; Drug Discovery and Development Centre (H3D), Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
  • Dam J; Drug Discovery and Development Centre (H3D), Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
  • Pawar K; Drug Discovery and Development Centre (H3D), Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
  • Taylor D; Drug Discovery and Development Centre (H3D), Division of Clinical Pharmacology, University of Cape Town, Rondebosch 7701, South Africa.
  • Lawrence N; Drug Discovery and Development Centre (H3D), Division of Clinical Pharmacology, University of Cape Town, Rondebosch 7701, South Africa.
  • Brunschwig C; Drug Discovery and Development Centre (H3D), Division of Clinical Pharmacology, University of Cape Town, Rondebosch 7701, South Africa.
  • Gibhard L; Drug Discovery and Development Centre (H3D), Division of Clinical Pharmacology, University of Cape Town, Rondebosch 7701, South Africa.
  • Njoroge M; Drug Discovery and Development Centre (H3D), Division of Clinical Pharmacology, University of Cape Town, Rondebosch 7701, South Africa.
  • Reader J; Department of Biochemistry, Genetics and Microbiology, Institute for Sustainable Malaria Control, University of Pretoria, Hatfield, Pretoria 0028, South Africa.
  • van der Watt M; Department of Biochemistry, Genetics and Microbiology, Institute for Sustainable Malaria Control, University of Pretoria, Hatfield, Pretoria 0028, South Africa.
  • Wicht K; Drug Discovery and Development Centre (H3D), Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
  • de Sousa ACC; Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
  • Okombo J; Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
  • Maepa K; Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
  • Egan TJ; Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
  • Birkholtz LM; Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa.
  • Basarab GS; Department of Biochemistry, Genetics and Microbiology, Institute for Sustainable Malaria Control, University of Pretoria, Hatfield, Pretoria 0028, South Africa.
  • Wittlin S; Drug Discovery and Development Centre (H3D), Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
  • Fish PV; Swiss Tropical and Public Health Institute ,Socinstrasse 57, 4002 Basel, Switzerland.
  • Street LJ; University of Basel, 4002 Basel, Switzerland.
  • Duffy J; Alzheimer's Research UK, UCL Drug Discovery Institute, The Cruciform Building, University College London, Gower Street, London WC1E 6BT, U.K.
  • Chibale K; Drug Discovery and Development Centre (H3D), Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
J Med Chem ; 63(21): 13013-13030, 2020 11 12.
Article in En | MEDLINE | ID: mdl-33103428
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Full text: 1 Collection: 01-internacional Health context: 3_ND Database: MEDLINE Main subject: Plasmodium falciparum / Pyridines / Protozoan Proteins / Hemeproteins / Imidazoles / Antimalarials Type of study: Diagnostic_studies / Prognostic_studies Limits: Animals Language: En Journal: J Med Chem Year: 2020 Document type: Article
Fulltext
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Full text: 1 Collection: 01-internacional Health context: 3_ND Database: MEDLINE Main subject: Plasmodium falciparum / Pyridines / Protozoan Proteins / Hemeproteins / Imidazoles / Antimalarials Type of study: Diagnostic_studies / Prognostic_studies Limits: Animals Language: En Journal: J Med Chem Year: 2020 Document type: Article